在固体阶段,并行合成维生素D的图书馆
I Hijikuro1, T Doi, T Takahashi
1Department of Applied Chemistry, Graduate School of Science and Engineering, Tokyo Institute of Technology, 2-12-1 Ookayama, Meguro, Tokyo 152-8552, Japan.
Journal of the American Chemical Society
|July 18, 2001
概括
这项研究提出了一种有效的固体相合成维生素D的类似物. 新的策略使维生素D的平行合成和多样化成为可能.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 合成化学 合成化学
背景情况:
- 维生素D ((3) 和它的类似物在各种生物过程中至关重要.
- 开发有效的维生素D类别的合成途径对于研究和治疗应用至关重要.
研究的目的:
- 为维生素D及其类型开发高效的固体相合成策略.
- 为了使维生素D的平行合成和多样化,用于更广泛的应用.
主要方法:
- 对于维生素D的类似物,开发了两种不同的固体相合成策略.
- 将CD环前体固定在固体支上 (PS-DES树脂,硫酸盐树脂).
- 利用霍纳-瓦兹沃斯-埃蒙斯反应,Cu (I) 催化格里格纳德试剂用于同时引入和切割侧链,以及用于并行合成的组合化学.
主要成果:
- 在高效率的固体支上成功合成了维生素D系统.
- 开发了针对11-基相似物和其他合成相似物的具体策略.
- 通过分割和池方法和射频编码的组合化学,证明了多种维生素D类型的并行合成.
- 还实现了各种A环构建块的高效准备.
结论:
- 描述的固体相合成为产生维生素D的类似物提供了一种高效和多功能方法.
- 该方法促进了并行合成和多样化,加速了新型维生素D的发现.
- 这种方法为进一步研究维生素D化学和药理学提供了有价值的基石.
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